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(+)-麦角酸作为一种安全稳定的局部光保护剂的有前途的候选物。

(+)-Usnic Acid as a Promising Candidate for a Safe and Stable Topical Photoprotective Agent.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

Department of Pharmaceutical Biochemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

出版信息

Molecules. 2021 Aug 28;26(17):5224. doi: 10.3390/molecules26175224.

Abstract

The study aimed to examine whether usnic acid-a lichen compound with UV-absorbing properties-can be considered as a prospective photoprotective agent in cosmetic products. Moreover, a comparison of two usnic acid enantiomers was performed to preselect the more effective compound. To meet this aim, an in vitro model was created, comprising the determination of skin-penetrating properties via skin-PAMPA assay, safety assessment to normal human skin cells (keratinocytes, melanocytes, fibroblasts), and examination of photostability and photoprotective properties. Both enantiomers revealed comparable good skin-penetrating properties. Left-handed usnic acid was slightly more toxic to keratinocytes (IC 80.82 and 40.12 µg/mL, after 48 and 72 h, respectively) than its right-handed counterpart. The latter enantiomer, in a cosmetic formulation, was characterized by good photoprotective properties and photostability, comparable to the UV filter octocrylene. Perhaps most interestingly, (+)-usnic acid combined with octocrylene in one formulation revealed enhanced photoprotection and photostability. Thus, the strategy can be considered for the potential use of (+)-usnic acid as a UV filter in cosmetic products. Moreover, the proposed model may be useful for the evaluation of candidates for UV filters.

摘要

本研究旨在探讨地衣酸(一种具有紫外线吸收特性的化合物)是否可被视为化妆品中的潜在光保护剂。此外,还对两种地衣酸对映异构体进行了比较,以预先选择更有效的化合物。为了实现这一目标,创建了一个体外模型,包括通过皮肤 PAMPA 测定法测定皮肤穿透特性、对正常人体皮肤细胞(角质形成细胞、黑素细胞、成纤维细胞)的安全性评估,以及检查光稳定性和光保护特性。两种对映异构体均显示出相当好的皮肤穿透特性。左式地衣酸对角质形成细胞的毒性略高于右式地衣酸(分别在 48 和 72 小时后,IC 80.82 和 40.12 µg/mL)。后者对映异构体在化妆品配方中具有良好的光保护和光稳定性,与紫外线滤光剂辛基三嗪酮相当。也许最有趣的是,(+)-地衣酸与辛基三嗪酮在一种配方中联合使用时,显示出增强的光保护和光稳定性。因此,可以考虑将(+)-地衣酸作为一种紫外线滤光剂用于化妆品中。此外,所提出的模型可能有助于评估紫外线滤光剂候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b4a0/8433837/3de16053a05d/molecules-26-05224-g001.jpg

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